Issue Information – TOC

Drug transporters are of critical importance as they regulate pharmacokinetic properties of drugs (absorption, distribution, and elimination) and can cause the development of cellular drug resistance through decreased uptake or increased efflux of drugs in therapeutic target organs. The ubiquitous distribution of these transporters and their role in the cellular uptake and efflux of xenobiotics suggest that transporters play a crucial role in the therapeutic effects of multiple clinically important drugs. This issue of CPT highlights recent advances into how transporters impact on cellular sensitivity, absorption and disposition, toxicity, and efficacy profiles of drugs. Further understanding of the role of transporters in drug-drug interactions and identification of these proteins as possible therapeutic targets will contribute to improved treatment outcome of a wide variety of diseases.